Plural 1,2-diazoles (including Hydrogenated) Patents (Class 548/365.1)
  • Patent number: 10556868
    Abstract: The present invention relates to a method for synthesizing a compound of 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid, wherein including the steps of: (A) the diethyl ester compounds represented by the following Formula IV are reacted under the action of amine, alkali and carbonyl reagents to produce the acrylic diester compound represented by the following Formula I, wherein: (B) the above compound represented by the Formula I is reacted with a fluoride reagent, a Lewis acid and a methyl hydrazine to form a pyrazole ring-containing diester compound represented by the Formula II, (C) the heterocyclic-containing diester compound represented by the Formula II is reacted with a base to give 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic acid represented by the Formula III.
    Type: Grant
    Filed: September 29, 2016
    Date of Patent: February 11, 2020
    Assignee: ZHEJIANG YONGTAI TECHNOLOGY CO., LTD.
    Inventors: Renbao He, Yingmei Wang, Hongming Shao, Yizhong Jin
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Publication number: 20150112075
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Carl DeAMICIS, Kaitlyn GRAY, Yu ZHANG, Joseck M. MUHUHI
  • Patent number: 8975254
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 10, 2015
    Assignee: Orion Corporation
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 8940273
    Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: January 27, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
  • Publication number: 20140378474
    Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
  • Publication number: 20140364621
    Abstract: This disclosure concerns two novel electrically conducting organic oligomers: oligo(3-amino-1H-pyrazole-4-carbonitrile) or “oligo(AP-CN)” and oligo(4-nitro-1H-pyrazole-3-yl-amine) or “oligo(AP-NO2)”, and methods of making thereof.
    Type: Application
    Filed: May 16, 2014
    Publication date: December 11, 2014
    Applicant: The Government of the United States of America, as represented by the Secretary of the Navy
    Inventors: Brett D. Martin, Scott A. Trammell, Jeffrey R. Deschamps, Jawad Naciri, Jeffrey C. DePriest
  • Patent number: 8883689
    Abstract: A herbicide composition includes a fenoxaprop ester and a weak acid buffer system. The buffer system maintains the herbicidal composition at a pH in the range of 4 to 8. In one non-limiting embodiment, the fenoxaprop ester is fenoxaprop ethyl. The buffer system can include an amine-containing material, such as a tertiary amine. The herbicide composition can include other herbicides, such as weak acid herbicides, for example pyrasulfotole, bromoxynil, and/or bromoxynil esters and can include one or more safeners.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: November 11, 2014
    Assignee: Bayer CropScience LP
    Inventors: Tai-Teh Wu, Karen L. Eagles
  • Publication number: 20140303372
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 9, 2014
    Applicant: ABBVIE BHAMAS LTD.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20140296238
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: June 10, 2014
    Publication date: October 2, 2014
    Inventors: Henry YU, Thomas E. RICHARDSON, Robert James FOGLESONG, Lizbeth Celeste DESELM, Andreas GOUTOPOULOS
  • Publication number: 20140256771
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Publication number: 20140179733
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Publication number: 20140171420
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Pingchen Fan, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang, Dean Dragoli
  • Patent number: 8716485
    Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 6, 2014
    Assignee: Westfälishe Wilhelms-Universität Münster
    Inventors: Julia Neumann, Mamta Suri, Frank Glorius
  • Patent number: 8642508
    Abstract: The present invention is directed to the discovery, isolation, identification and methods of synthesis of a novel chemical complex that can be used to stabilize mixtures of different chemical compounds, and in particular mixtures of different herbicidal compounds.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: February 4, 2014
    Assignee: Bayer Cropscience LP
    Inventors: Tai-Teh Wu, Karen L. Eagles, Michael W. Edenfield
  • Publication number: 20140005231
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein L is —C(R12a)R12b—C(R13a)R13b—, wherein the carbon atom bonded to R12a and R12b is also bonded to the carboxamide nitrogen atom in Formula 1; or 1,2-phenylene optionally substituted with up to 4 substituents independently selected from halogen and C1-C2 alkyl; and A, Z, R1, R2, n, G and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are methods for controlling a phytophagous nematode comprising contacting the nematode or its environment with a nematocidally effective amount of a compound of Formula 1 wherein L is —C(R12a)R12b—C(R13a)R13b; and A, Z, R1, R2, n, G and Q are as defined in the disclosure.
    Type: Application
    Filed: June 19, 2013
    Publication date: January 2, 2014
    Inventors: JAMES FRANCIS BEREZNAK, Steven Gutteridge, Ravisekhara P. Reddy, Andrew Edmund Taggi, Matthew James Campbell, Moumita Kar, Johan A. J. Desaeger
  • Publication number: 20130274227
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 14, 2013
    Publication date: October 17, 2013
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20130177529
    Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.
    Type: Application
    Filed: November 15, 2012
    Publication date: July 11, 2013
    Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
  • Patent number: 8481494
    Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: July 9, 2013
    Inventors: Thomas Schrader, Katrin Hochdörffer, Julia März-Berberich, Luitgard Nagel-Steger, Gal Bitan, Sharmistha Sinha
  • Publication number: 20130165452
    Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
    Type: Application
    Filed: February 22, 2013
    Publication date: June 27, 2013
    Applicant: PFIZER INC.
    Inventor: Pfizer Inc.
  • Publication number: 20130131327
    Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: Mallinckrodt LLC
    Inventor: Mallinckrodt LLC
  • Publication number: 20130059833
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.
    Type: Application
    Filed: August 30, 2012
    Publication date: March 7, 2013
    Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Patent number: 8372379
    Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: February 12, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
  • Publication number: 20130012715
    Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.
    Type: Application
    Filed: March 23, 2011
    Publication date: January 10, 2013
    Applicant: WESTFAELISCHE WILHELMS UNIVERSITAET MUENSTER
    Inventors: Julia Neumann, Mamta Suri, Frank Glorius
  • Publication number: 20120316150
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.
    Type: Application
    Filed: June 18, 2012
    Publication date: December 13, 2012
    Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Publication number: 20120270795
    Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: January 26, 2010
    Publication date: October 25, 2012
    Inventors: Thomas Schrader, Katrin Hochdörffer, Julia März-Berberich, Luitgard Nagel-Steger, Gal Bitan, Sharmistha Sinha
  • Publication number: 20120238752
    Abstract: Provided is a colored photosensitive curing composition useful for color filters in primary colors, including blue, green, and red, having a high molar absorption coefficient and allowing a reduction in film thickness and superior color purity and fastness. A colored photosensitive curing composition, comprising, as its colorant, a dipyrromethene-based metal complex compound obtained from a metal or metal compound and a dipyrromethene-based compound represented by the following Formula (I): wherein in Formula (I), R1 to R6 each independently represent a hydrogen atom or a substituent group; and R7 represents a hydrogen or halogen atom, or an alkyl, aryl or heterocyclic group.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 20, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Yuki MIZUKAWA, Ryoji GOTO, Hideki TAKAKUWA, Masashi OGIYAMA, Toru FUJIMORI
  • Publication number: 20120225867
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: October 27, 2010
    Publication date: September 6, 2012
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 8227619
    Abstract: The invention relates to a process for the preparation of fungicidally active compounds such as tricyclic amine derivatives (I). The process involves coupling of a carboxylic 5 acid e.g. a compound of formula (II) with an aniline, e.g. a compound of formula (III) in the presence of a boronic acid catalystor an antimony catalyst (II)(III)(I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Het are defined in the specification.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: July 24, 2012
    Assignee: Syngenta Limited
    Inventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, George Robert Hodges
  • Patent number: 8222410
    Abstract: Provided is an azo pigment represented by the following general formula (1), a tautomer of the azo pigment, and a salt or a hydrate thereof: wherein Q represents the non-metallic atoms necessary to complete a 5- to 7-membered heterocyclic group, W represents an alkoxy group, an amino group, an alkyl group, or an aryl group, X1 and X2 each independently represents a hydrogen, an alkyl group, an acyl group, an alkylsulfonyl group, or an arylsulfonyl group, R1 represents a hydrogen or a substituent, R2 represents a heterocyclic group, n represents an integer of from 1 to 4 and the general formula (1) represents a dimer formed through Q, W, X1, X2, R1, or R2 when n=2, a trimer formed through Q, W, X1, X2, R1, or R2 when n=3, and a tetramer formed through Q, W, X1, X2, R1, or R2 when n=4.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: July 17, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Keiichi Tateishi, Shinya Hayashi, Masaru Takasaki, Nobuo Seto
  • Publication number: 20120108424
    Abstract: The present invention is directed to the discovery, isolation, identification and methods of synthesis of a novel chemical complex that can be used to stabilize mixtures of different chemical compounds, and in particular mixtures of different herbicidal compounds.
    Type: Application
    Filed: July 11, 2008
    Publication date: May 3, 2012
    Inventors: Tai-Teh Wu, Karen L. Eagles, Michael W. Edenfield
  • Patent number: 8168796
    Abstract: There are provided novel fluorescent agents, such as pyrazoline compounds represented by formula (I): (wherein R1, R2 and R3 are as defined in the specification), having an ethynyl group in the molecule, which have high absorptivity in the ultraviolet-visible short wavelength range (for example, 350 nm-420 nm).
    Type: Grant
    Filed: January 19, 2009
    Date of Patent: May 1, 2012
    Assignee: Nippon Chemical Works Co., Ltd.
    Inventors: Kazuhiko Mizuno, Hideyuki Takagaki, Hirokazu Iwahashi, Kaname Inoue
  • Publication number: 20110245157
    Abstract: This invention provides for dimeric1-arylpyrazole compounds, of formulas (I), (II), and (III): or salts thereof, and the use of these compounds against ectoparasites such as insects, arthropods and acarina. The resulting compounds may be used in veterinary formulations such as, for example, spot-on and pour-on formulations, which may be used for treatment, controlling and preventing of parasitic infections in warm-blooded animals and birds.
    Type: Application
    Filed: November 18, 2009
    Publication date: October 6, 2011
    Inventor: Charles Q. Meng
  • Publication number: 20110230445
    Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
    Type: Application
    Filed: May 26, 2011
    Publication date: September 22, 2011
    Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
  • Patent number: 8008278
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: August 30, 2011
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes
  • Patent number: 8003650
    Abstract: Disclosed is a hydrazine compound represented by the formula (1) below, which has an excellent control activity against a harmful arthropod. (1) (In the formula, R1, R5, R6 and R7 represent a hydrogen atom or the like; R2 and R3 are bonded together at their ends to form a 5- to 8-membered ring together with two nitrogen atoms; R4 represents a halogen atom or the like; J represents 1-(3-chloro-2-pyridyl)-3-bromo-1H-pyrazol-5-yl group or the like; and M represents a hydrogen atom, an optionally halogenated C1-C6 alkyl group, or the like.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: August 23, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Markus Jachmann, Hiroshi Ikegami, Yoshihiko Nokura
  • Patent number: 7994341
    Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: August 9, 2011
    Assignee: Syngenta Limited
    Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi, Fanny Giordano, Martin Zeller, Gottfried Seifert, Shailesh Shah, Neil George, Ian Kevin Jones, Paul Edward Bonnett
  • Publication number: 20110144080
    Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.
    Type: Application
    Filed: December 23, 2004
    Publication date: June 16, 2011
    Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITAL
    Inventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
  • Patent number: 7947680
    Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: May 24, 2011
    Assignee: H. Lundbeck A/S
    Inventors: Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
  • Publication number: 20110092539
    Abstract: The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Application
    Filed: June 3, 2009
    Publication date: April 21, 2011
    Inventors: Jonathan Gillespie, Craig Jamieson, Zoran Rankovic
  • Patent number: 7923004
    Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.
    Type: Grant
    Filed: October 15, 2007
    Date of Patent: April 12, 2011
    Assignee: XTL Biopharmaceuticals Ltd.
    Inventors: Guolin Li, Reza Fathi, Zhen Yang, Yun Liao, Qiang Zhu, Angela Lam, Anthony Sandrasagra, Kenneth Nawoschik, Hyun-Joon Cho, Jie Cao, Wu Ruoqiu, C. Richard Wobbe, Yixin Liu
  • Patent number: 7893611
    Abstract: There is provided a novel luminescent metal complex. A metal complex having a composition of [(PtII)2(MI)2(X)2(L)4(LH)2], where MI denotes AgI, AuI or CuI, X denotes Cl, Br or I, L denotes a structure represented by the formula (1), and LH denotes a structure represented by the formula (2).
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: February 22, 2011
    Assignee: Nagasaki University
    Inventors: Keisuke Umakoshi, Seiji Akatsu, Masayoshi Onishi, Shoji Ishizaka, Noboru Kitamura
  • Publication number: 20100249091
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally subs
    Type: Application
    Filed: September 17, 2009
    Publication date: September 30, 2010
    Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Publication number: 20100144793
    Abstract: The present invention relates to compounds of the general formula (I) wherein (formula 2) independently represents a single bond or a double bond, represents a linking group A and A? are each independently a 5- to 7-membered heterocyclic ring, wherein the heterocyclic rings A und A? are optionally substituted by one or more substituents, selected from C1-6 alkyl, C3-6 cycloalkyl, optionally substituted phenyl, optionally substituted heteroaryl, C1-4 alkylene-(optionally substituted phenyl) and C1-4 alkylene-(optionally substituted heteroaryl), or two substituents may be joined to form an optionally substituted, saturated, unsaturated or aromatic 5- to 7-membered ring which is fused with the heterocyclic ring A or A?, and wherein the heterocyclic rings A und A? may contain in addition to the units X, X?, Y and Y? one or more heteroatoms, selected from N, NR, S and Ol wherein R is selected from H and C1-4 alkyl; the units X and X? are each independently a H-bond acceptor; and the units Y and Y? are each indepen
    Type: Application
    Filed: November 23, 2007
    Publication date: June 10, 2010
    Applicant: AC IMMUNE SA
    Inventors: Wolfgang Froestl, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas Muhs, Maria Pihlgren Bosch
  • Patent number: 7728018
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: June 1, 2010
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Patent number: 7696199
    Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
    Type: Grant
    Filed: August 29, 2005
    Date of Patent: April 13, 2010
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, María Montserrat Contijoch-Llobet
  • Publication number: 20100074842
    Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
    Type: Application
    Filed: November 23, 2007
    Publication date: March 25, 2010
    Inventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
  • Publication number: 20100063063
    Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
    Type: Application
    Filed: September 9, 2009
    Publication date: March 11, 2010
    Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
  • Patent number: 7662961
    Abstract: The invention relates to bis-5-pyrazolyl derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: February 16, 2010
    Assignee: Merial Limited
    Inventors: Stefan Schnatterer, Michael Maier, Friederike Lochhaas, Werner Knauf, Karl Seeger
  • Patent number: 7592338
    Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: September 22, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski